Blar i forfatter "Riss, Patrick"

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    • An Acylation-Finkelstein Approach to Radioiodination of Bioactives: The Role of Amide Group Anchimeric Assistance 

      Fjellaksel, Richard; Dugalic, Damir; Demissie, Taye Beyene; Riss, Patrick; Hjelstuen, Ole Kristian; Sundset, Rune; Hansen, Jørn H (Journal article; Tidsskriftartikkel; Peer reviewed, 2018-02-28)
      Herein, we report a straightforward sequential acylation‐Finkelstein approach to achieve iodination of amine containing bioactives. The utility was demonstrated by successful radiolabelling with <sup>123</sup>I in high radiochemical yield. Moreover, microwave‐assisted Finkelstein reaction can be employed to enhance conversion and reaction rates to obtain the desired iodides. The method is of interest ...

    • Discovery of a lead brain-penetrating gonadotropin-releasing hormone receptor antagonist with saturable binding in brain 

      Bekker, Roberto Bartholomeus Wilhelmus; Fjellaksel, Richard; Hjornevik, Trine; Nuruddin, Syed; Rafique, Waqas; Hansen, Jørn H; Sundset, Rune; Haraldsen, Ira Hebold; Riss, Patrick (Journal article; Tidsskriftartikkel; Peer reviewed, 2020-07-16)
      We report the synthesis, radiosynthesis and biological characterisation of two gonadotropin‐releasing hormone receptor (GnRH−R) antagonists with nanomolar binding affinity. A small library of GnRH−R antagonists was synthesised in 20–67 % overall yield with the aim of identifying a high‐affinity antagonist capable of crossing the blood–brain barrier. Binding affinity to rat GnRH−R was determined by ...

    • Evaluation by metabolic profiling and in vitro autoradiography of two promising GnRH‐receptor ligands for brain SPECT imaging 

      Fjellaksel, Richard; Moldes-Anaya, Angel; Vasskog, Terje; Oteiza, Ana; Martin-Armas, Maria Montserrat; Hjelstuen, Ole Kristian; Hansen, Jørn H; Riss, Patrick; Sundset, Rune (Journal article; Tidsskriftartikkel; Peer reviewed, 2019-12-18)
      The increased expression of gonadotropin releasing hormone receptor (GnRH‐R) in brain has been strongly linked to Alzheimer disease. Therefore, the development of radiolabeled imaging agents for GnRH‐R is relevant for early diagnosis of Alzheimer disease. We have recently disclosed the discovery of two promising compounds displaying nanomolar‐range affinity for the GnRH‐R. In the present study, a ...

    • First in vivo evaluation of a potential SPECT brain radiotracer for the gonadotropin releasing hormone receptor 

      Fjellaksel, Richard; Oteiza, Ana; Martin, armas maria montserrat; Riss, Patrick; Hjelstuen, Ole Kristian; Kuttner, Samuel; Hansen, Jørn H; Sundset, Rune (Journal article; Tidsskriftartikkel; Peer reviewed, 2018-11-09)
      <p><i>Objectives</i>: In vivo evaluations of a gonadotropin releasing hormone-receptor single photon emission computed tomography radiotracer for non-invasive detection of gonadotropin releasing homone-receptors in brain.</p> <p><i>Results</i>: We have used a simple, robust and high-yielding procedure to radiolabel an alpha-halogenated bioactive compound with high radiochemical yield. Literature ...

    • Small molecule piperazinyl-benzimidazole antagonists of the gonadotropin-releasing hormone (GnRH) receptor 

      Fjellaksel, Richard; Boomgaren, Marc; Sundset, Rune; Haraldsen, Ira Hebold; Hansen, Jørn H; Riss, Patrick (Journal article; Tidsskriftartikkel; Peer reviewed, 2017-08-14)
      In this communication, we report the synthesis and characterization of a library of small molecule antagonists of the human gonadotropin releasing hormone receptor based upon the 2-(4-<i>tert</i>-butylphenyl)-4-piperazinyl-benzimidazole scaffold <i>via</i> Cu-catalysed azide alkyne cycloaddition. Our main purpose was to find a more soluble compound based on the WAY207024 lead with nanomolar potency ...